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Musculoskeletal MBCHB > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Give examples of NSAIDs

A

ibuprofen, naproxen, diclofenac

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2
Q

What are the main indications for NSAID use?

A
  • Inflammatory arthritis
  • Mechanical MSK pain
  • Pleuritic/pericardial pain
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3
Q

What is the mechanism of action of NSAIDs?

A

Most NSAIDs act as nonselective inhibitors of the cyclooxygenase (COX) enzymes

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4
Q

What are some contraindications for NSAIDs?

A

Contraindicated in peptic ulcer disease

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5
Q

What are some side effects of NSAIDs?

A
  • GI - dyspepsia, oesophagitis, gastritis, peptic ulcer, bowel ulceration
  • Renal impairment
  • Increased cardiovascular risk
  • Fluid retention
  • Wheeze - caution in asthma
  • Rash
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6
Q

What is the administration method for NSAIDs?

A

PO

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7
Q

What are the main indications for methotrexate?

A
  • First line DMARD
  • Used in RA, psoriatic arthritis, connective tissue disease, and vasculitis
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8
Q

What is the mechanism of action for methotrexate?

A

Folate antagonist, mode of action unknown

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9
Q

What are the contraindications of methotrexate?

A
  • Teratogenic - must be stopped in females at least 3 months before conception
  • FBC + LFTs should be monitored
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10
Q

What are some adverse effects of methotrexate?

A
  • Leukopenia/thrombocytopenia (due to suppression of bone marrow)
  • Hepatitis/cirrhosis (alcohol intake must be limited)
  • Pneumonitis
  • Rash/mouth ulcers
  • Nausea/diarrhoea
  • Co-prescribed with folic acid to reduce some adverse effects
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11
Q

What is the route of administration for methotrexate?

A

PO or SC

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12
Q

What are the main indications for leflunomide?

A
  • DMARD
  • Similar efficacy to methotrexate
  • Used in RA, psoriatic arthritis, connective tissue disease, and vasculitis
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13
Q

What is the mechanism of action of methotrexate?

A

Pyrimidine synthesis inhibitor that works by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase

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14
Q

What are some contraindications for methotrexate?

A
  • Teretogenic
  • Very long half life - requires wash out
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15
Q

What are the adverse effects of leflunomide?

A
  • Leukopenia/thrombocytopenia (due to suppression of bone marrow)
  • Hepatitis/cirrhosis (alcohol intake must be limited)
  • Pneumonitis
  • Rash/mouth ulcers
  • Nausea/diarrhoea
  • Co-prescribed with folic acid to reduce some adverse effects
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16
Q

What is the route of administration for leflunomide?

A

PO

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17
Q

What are the main indications of sulfasalazine?

A
  • DMARD
  • Often used in combination with methotrexate in early inflammatory arthritis
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18
Q

What is the mechanism of action of sulfasalazine?

A

Precise MOA is unknown

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19
Q

What are the contraindications of sulfasalazine?

A
  • Use with caution in acute porphyrias
  • FBC + LFTs should be monitored
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20
Q

What are the adverse effects of sulfasalazine?

A
  • Nausea
  • Rash/mouth ulcers
  • Neutropenia
  • Hepatitis
  • Reversible oligozoospermia
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21
Q

What is the route of administration for sulfasalazine?

A

PO

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22
Q

What are the main indications for hydroxychloroquine?

A
  • DMARD
  • Efficacy for arthritis weaker than that of methotrexate
    • No effect on joint damange - patients report decrease in malaise, myalgia when taken alongside e.g. methotrexate
  • Used in connective tissue diseases - SLE, Sjogren’s syndrome
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23
Q

What is the mechanism of action of hydroxychloroquine?

A

Precise MOA is unknown

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24
Q

What are the contraindications of hydroxychloroquine?

A

Use with caution in acute porphyrias

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25
Q

What are the adverse effects of hydroxychloroquine?

A

Retinopathy (recognised but rare) - annual optometry check ups

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26
Q

What is the route of administration for hydroxychloroquine?

A

PO

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27
Q

What are the main indications of Anti-TNF therapy?

A
  • Licensed for RA, psoriatic arthritis and ankylosing spondylitis
  • Because of their higher cost, in the UK tend to be used after a failure of 2 DMARDs or in ankylosing spondylitis 2 NSAIDs
28
Q

What is the mechanism of action for Anti-TNF therapy?

A

Tumor necrosis factor (TNF)-α is a potent pro-inflammatory and pathological cytokines in inflammatory diseases

29
Q

What are the contraindications of anti-TNF therapy?

A
  • No evidence of biologics causing foetal abnormalities but is currently unknown whether there is any long term effect on the child’s immune system
    • Certolizumab is the only anti-TNF licensed in pregnancy/breastfeeding as it is unable to cross the placental barrier due to its pergolated component
    • Other anti-TNFs thought to be safe in the first 2 trimesters but usually advised to stop in 3rd trimester
30
Q

What are the adverse effects of anti-TNF therapy?

A
  • Risk of infection (especially TB)
  • May increase risk of malignancy (especially skin cancer)
  • Contraindicated in pulmonary fibrosis, heart failure, others
31
Q

What is the route of administration of anti-TNF therapy?

A

SC

32
Q

What is rituximab?

A

monoclonal antibody against B (CD20) lymphocytes

33
Q

What is toclizumab?

A

monoclonal antibody that inhibits IL-6

34
Q

What is abataceot?

A

CTLA-4 Ig - blocks full activation of T lymphocytes

35
Q

What is ustekinamab?

A

monoclonal antibody inhibits IL12 and IL23

36
Q

What is secukinimab?

A

monoclonal antibody that inhibits IL-17

37
Q

What are the main indicators in MSK for corticosteroids?

A
  • Inflammatory arthritis
  • Polymyalgia rheumatica/giant cell arteritis
  • Vasculitis
38
Q

What is the mechanism of action for corticosteroids?

A

Increase transcription of anti-inflammatory proteins and decreases transcription of pro-inflammatory proteins

39
Q

What are some contraindications of corticosteroids?

A
  • Use lowest possible dose for as short a time as possible
  • Consider steriod sparing agents
  • Osteoporosis prophylaxis
  • Monitor cardiovascular risk factors and for development of diabetes
40
Q

What are adverse effects of corticosteroids?

A
  • Weight gain - centripetal obesity
  • Muscle wasting
  • Skin atrophy
  • Osteoporosis
  • Diabetes
  • Hypertension
  • Cataract
  • Glaucoma
  • Fluid retension
  • Adrenal suppression
  • Immunosuppression
  • Avascular necrosis of the femoral head
41
Q

How can corticosteroids be administered?

A

PO
Intra-articular
IM
IV

42
Q

What are the main indications for allopurinol?

A

Gout prophylaxis (first line)

43
Q

What is the mechanism of action for allopurinol?

A

Xanthine oxidase inhibitor

44
Q

What are the contraindications for allopurinol?

A
  • Contraindicated in renal impairment
  • Gout prophylaxis should be started 4-6 weeks after acute attack and requires cover with NSAIDs for first 6 months (or colchicine/steroids) as rapid reduction in uric acid level may result in further exacerbation of gout
45
Q

What are the adverse effects of allopurinol?

A
  • Rash (vasculitis)
  • Azathioprine interaction
  • Marow aplasia (rare)
46
Q

How is allopurinol administered?

A

PO

47
Q

What are the main indications of febuxostat?

A

Gout prophylaxis when allopurinol not tolerated/contraindicated

48
Q

What is the mechanism of action of febuxostat?

A

Xanthine oxidase inhibitor

49
Q

What are the contraindications of febuxostat?

A
  • Contraindicated in ischaemic heart disease
  • Gout prophylaxis should be started 4-6 weeks after acute attack and requires cover with NSAIDs for first 6 months (or colchicine/steroids) as rapid reduction in uric acid level may result in further exacerbation of gout
50
Q

What is a side effect of febuxostat?

A

Rash (vasculitis)

51
Q

What are examples of oral bisphosphonates?

A

Alendronate, risedronate, etidronate

52
Q

What are the main indications for oral bisphosphonates?

A
  • First line in majority of patients with osteoporosis
    • Consider treatment with when T score </= -2.5
    • If ongoing steroid requirement >/= 7.5mg prednisolone for 3 months or more or if there is a prevalent vertebral fracture, consider treatment with T score < 1.5
  • Paget’s disease of bone
  • May have some benefit in patients with osteogenesis imperfecta in teenage years
53
Q

What is the mechanism of action of oral bisphosphonates?

A
  • Analogues of pyrophosphate that absorb onto bone within the matrix; ingested by osteoclasts leading to cell death thereby inhibiting bone resorption
  • Prevent bone loss at all sites vulnerable to osteoporosis
54
Q

What are the adverse effects of oral bisphosphonates?

A
  • 5-10 year course to reduce risk of (rare) long-term side effects associated with duration of use
    • Osteonecrosis of the jaw
    • Oesophageal carcinoma
    • Atypical fractures
55
Q

What are the main indications for zoledronic acid?

A

Second line for majority of patients with osteoporosis e.g. patients with side effects with oral bisphonates

56
Q

What are the adverse effects of zoledronic acid?

A

1/3 acute phase reaction with first infusion - manage with paracetamol

57
Q

What are the main indications for Desunomab?

A

Another second line alternative to oral bisphosphonates in patients with osteoporosis

58
Q

What is the mechanism of action of Desunomab?

A
  • Monoclonal antibody which reduces osteoclast activity
  • Binding to RANKL (receptor activator of nuclear factor-kB ligand) prevents the activation of RANK which inhibits development and activity of osteoclasts, decreasing bone resorption and increasing bone density
59
Q

What are the adverse effects of Desunomab?

A
  • Hypocalcaemia
  • Eczema
  • Cellulitis
60
Q

How is Desunomab administered?

A

S/C injection 6 monthly

61
Q

What are the main indications of teriparatide?

A
  • Recommended to reduce risk of vertebral and non-vertebral fractures in postmenopausal women with severe osteoporosis
  • Recommended over oral bisphosphate in postmenopausal women with at least 2 moderate or 1 severe low trauma vertebral fracture to prevent vertebral fracture
62
Q

What is the mechanism of action for teriparatide?

A

Recombinant parathyroid hormone; stimulates bone growth rather than reduces bone loss (anabolic)

63
Q

How is teriparatide administered?

A

Daily S/C injection

64
Q

What are the main indications of romosozumab?

A

Recommended for postmenopausal women with severe osteoporosis who have had a fragility fracture and are at imminent risk of further fracture (24 months)

65
Q

What is the mechanism of action for romosozumab?

A

Monoclonal antibody that binds to and inhibits sclerostin (sclerostin inhibits bone formation) to increase bone formation and reduce bone resorption

66
Q

What are the contraindications of romosozumab?

A

Previous MI/CVA

67
Q

How is romosozumab administered?

A

Monthly SC injection for 12 months, then followed by anti-resorptive

Musculoskeletal MBCHB (21 decks)

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